Tricyclic HIV integrase inhibitors: Potent and orally bioavailable C5-aza analogs

A series of C5-aza tricyclic HIV integrase inhibitors was prepared. A highly potent and orally bioavailable compound (compound 9) was identified and selected for development.

The design and preparation of highly potent tricyclic HIV integrase inhibitors are reported. The lead compound has shown good oral bioavailability in both rat and dog.Figure optionsDownload as PowerPoint slide